IDO-TDO Inhibitor Compounds for Immunosuppression Treatment

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Solution Overview

Problem

Current IDO inhibitors have limitations in efficacy for treating diseases mediated by indoleamine 2,3-dioxygenase (IDO), and there is a need for new IDO modulators that can effectively target IDO and tryptophan-2,3-dioxygenase (TDO) to address immunosuppression and cancer progression.

Innovation Solution

Development of compounds represented by formula (Ia3) that modulate IDO activity, potentially inhibiting both IDO and TDO, which can be used in pharmaceutical compositions to treat various diseases by reversing immunosuppression and enhancing T cell activation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current IDO inhibitors are used to treat IDO-mediated diseases, then some therapeutic effect is achieved, but efficacy is limited

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidbroad-spectrum activity against IDO and TDO
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent develops compounds that can inhibit both IDO and TDO enzymes, transforming a single-function inhibitor into a multi-function agent. This is achieved through molecular design that allows the compound to bind to and inhibit both tryptophan-2,3-dioxygenase and indoleamine-2,3-dioxygenase, thereby addressing the limitation of current inhibitors that only target IDO with limited efficacy

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Productivity

If traditional chemotherapy and radiotherapy are used to treat cancer, then tumor cells can be eliminated, but tumor cells can escape by regenerating primary tumor growth and seeding distant metastasis

Engineering Contradiction:
Improvetumor elimination rateVSAvoidlong-term success rate
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent introduces immunotherapy as an intermediary mechanism between traditional chemotherapy/radiotherapy and tumor elimination. By modulating IDO activity, the compounds enhance the immune system's ability to recognize and eliminate tumor cells, preventing tumor escape and metastasis while working synergistically with traditional treatments to improve long-term success rates

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentEP3215142B1Immunoregulatory agents
Publication Date: 2021.03.24 FLEXUS BIOSCI
  • EP3215142B1 patent drawingFigure 1A
  • EP3215142B1 patent drawingFigure 1B
  • EP3215142B1 patent drawingFigure 1C

AI summary

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3- dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.